Patents Examined by David K O'Dell
  • Fluorinated derivatives of 3-hydroxypyridin-4-ones
    Patent number: 9938240
    Abstract: Provided are compounds of Formula I which are derivatives of 3-Hydroxypyridin-4-ones. The compounds may be used in treatment of a medical condition related to a toxic concentration of iron. The compounds may be used for preparation of a medicament for treatment of a medical condition related to a toxic concentration of iron. The medical condition related to a toxic concentration of iron may be selected from the group consisting of: cancer, pulmonary disease, progressive kidney disease and Friedreich's ataxia.
    Type: Grant
    Filed: December 8, 2016
    Date of Patent: April 10, 2018
    Assignee: Apotex Inc.
    Inventors: Tim Fat Tam, Regis Leung-Toung, Yingsheng Wang, Yanqing Zhao, Tao Xin, Birenkumar Shah
  • 2,5,6,7-tetrasubstituted thiazolo[4,5-b]pyridine derivatives and use thereof
    Patent number: 9932355
    Abstract: Provided are a pharmaceutical composition containing a 2,5,6,7-tetrasubstituted thiazolo[4,5-b]pyridine derivative represented by Formula 1 as an active ingredient and a use thereof effective on a vascular inflammation-related infectious disease triggered by activity of HMGB1 protein. As investigating an anti-sepsis effect through a CLP-induced sepsis animal test that a sepsis survival rate is increased, it is identified that the pharmaceutical composition contains the 2,5,6,7-tetrasubstituted thiazolo[4,5-b]pyridine derivative or a pharmaceutically available salt thereof as an active ingredient to be used as a therapeutic agent for a vascular inflammatory disease and infectious disease including sepsis triggered by activity of HMGB1 protein.
    Type: Grant
    Filed: April 28, 2015
    Date of Patent: April 3, 2018
    Assignee: KYUNGPOOK NATIONAL UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATION
    Inventors: Taeho Lee, Jong-Sup Bae, Kyung-Sik Song, Sangkyu Lee, Kwang-Hyeon Liu, Wonhwa Lee, Doohyun Lee
  • Method for producing inhibitor of activated blood coagulation factor X (FXa)
    Patent number: 9920071
    Abstract: An object of the present invention is to provide a novel method for producing a compound, a salt thereof, or a hydrate of the compound or the salt, which is an FXa inhibitor. The object can be attained by a production method in which a production method via a compound represented by formula (1-1), etc., from a compound represented by the following formula (1-x), etc., is used for a method for producing a compound represented by the following formula (X), etc. [wherein X represents a halogen atom or the like, and R1 represents an optionally substituted phenyl group].
    Type: Grant
    Filed: February 13, 2015
    Date of Patent: March 20, 2018
    Assignee: Daiichi Sankyo Company, Limited
    Inventor: Tsuyoshi Ueda
  • Thieno [2,3-b] pyridines as multidrug resistance modulators
    Patent number: 9908893
    Abstract: The thieno[2,3-b]pyridines of general formula (I), wherein R1 is Me, C6H5, 3,4,5-(OMe)3C6H2, NH2; R2 is H, CN, COMe, COOC1-4alkyl, COOC2H4OMe, COOC2H4OPr(n); R3 is C6H4R6, 3,4-OCH2O—C6H3; 2-furanyl; R6 is 4-Cl, 4-NO2, 4-N(C1-4alkyl)2, 3-(C1-4alkyloxy), 4-(C1-4alkyloxy), 3,4-(C1-4alkyloxy)2, 3,4,5-(C1-4alkyloxy)3; R4 is NH2, NHCOMe; R5 is CN, COMe, COC6H4R7; CO-(2-naphthyl); R7 is H, 4-F, 4-Cl, 3-OMe, 4-OMe, 2,4-(OMe)2, 3,4,5-(OMe)3 as multidrug resistance modulators to increase the effectiveness of chemotherapy in cancer treatment.
    Type: Grant
    Filed: June 11, 2013
    Date of Patent: March 6, 2018
    Assignee: LATVIAN INSTITUTE OF ORGANIC SYNTHESIS
    Inventors: Ivars Kalvins, Aivars Krauze, Signe Grinberga, Laura Krasnova, Elina Jaschenko, Ilona Domracheva, Ilze Adlere, Zigmars Andzans, Irina Shestakova, Gunars Duburs
  • Pyrazolopyridine derivatives as modulators of TNF activity
    Patent number: 9902720
    Abstract: A series of substituted pyrazolo[1,5-a]pyridine derivatives, being potent modulators of human TNF? activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
    Type: Grant
    Filed: December 8, 2014
    Date of Patent: February 27, 2018
    Assignee: UCB BIOPHARMA SPRL
    Inventors: Daniel Christopher Brookings, Victoria Elizabeth Jackson, Boris Kroeplien
  • Sweet flavor modifier
    Patent number: 9902737
    Abstract: The present invention includes compounds having structural formula (I), or pharmaceutically acceptable salts, solvate, and/or ester thereof. These compounds are useful as sweet flavor modifiers. The present invention also includes compositions comprising the present compounds and methods of enhancing the sweet taste of ingestible compositions. Furthermore, the present invention provides methods for preparing the compounds.
    Type: Grant
    Filed: March 2, 2016
    Date of Patent: February 27, 2018
    Assignee: Senomyx, Inc.
    Inventors: Catherine Tachdjian, Xiao Qing Tang, Donald S. Karanewsky, Guy Servant, Xiaodong Li, Feng Zhang, Qing Chen, Hong Zhang, Timothy Davis, Vincent Darmohusodo, Melissa S. Wong, Victor Selchau
  • Piperidine compounds having multimodal activity against pain
    Patent number: 9902711
    Abstract: The present invention relates to compounds having dual pharmacological activity towards both the sigma (?) receptor, and the ?-opiod receptor and more particularly to piperidene compounds having this pharmacological activity, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
    Type: Grant
    Filed: December 19, 2014
    Date of Patent: February 27, 2018
    Assignee: LABORATORIOS DEL DR. ESTEVE S.A.
    Inventors: Félix Cuevas-Cordobés, Carmen Almansa-Rosales, Monica Garcia Lopez, Eva Maria Ayet Galcera, Maria Teresa Serafini Cabanes
  • Fused tricyclic compounds as Raf kinase inhibitors
    Patent number: 9895376
    Abstract: Provided are certain fused tricyclic compounds and salts thereof, compositions thereof, and methods of use therefor.
    Type: Grant
    Filed: January 22, 2016
    Date of Patent: February 20, 2018
    Assignee: BEIGENE, LTD.
    Inventors: Changyou Zhou, Shaohui Wang, Guoliang Zhang
  • Targeted nitroxide agents
    Patent number: 9890192
    Abstract: Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.
    Type: Grant
    Filed: November 17, 2015
    Date of Patent: February 13, 2018
    Assignee: University of Pittsburgh—Of the Commonwealth System of Higher Education
    Inventors: Peter Wipf, Marie-Celine Frantz
  • Fused pyrroledicarboxamides and their use as pharmaceuticals
    Patent number: 9884860
    Abstract: The present invention relates in fused pyrroledicarboxamides of the formula (I), in which R1 to R9, X, m and n are as defined in claims. The compounds of the formula (I) are inhibitors of the acid-sensitive potassium channel TASK-1 and suitable for the treatment of TASK-1 channel-mediated diseases such as arrhythmias, in particular atrial arrhythmias like atrial fibrillation or atrial flutter, and respiratory disorders, in particular sleep-related respiratory disorders like sleep apnea, for example.
    Type: Grant
    Filed: February 11, 2016
    Date of Patent: February 6, 2018
    Assignee: Sanofi
    Inventors: Laurent Bialy, Katrin Lorenz, Klaus Wirth, Klaus Steinmeyer, Gerhard Hessler
  • Cycloalkylamines as monoamine reuptake inhibitors
    Patent number: 9868718
    Abstract: The invention relates to novel cyclohexylamine derivatives and their use in the treatment and/or prevention of central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.
    Type: Grant
    Filed: September 30, 2014
    Date of Patent: January 16, 2018
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: Liming Shao, Fengjiang Wang, Scott Christopher Malcolm, Michael Charles Hewitt, Larry R. Bush, Jianguo Ma, Mark A. Varney, Una Campbell, Sharon Rae Engel, Larry Wendell Hardy, Patrick Koch, John E. Campbell
  • Processes of making and crystalline forms of a MDM2 inhibitor
    Patent number: 9855259
    Abstract: The present invention provides processes for making 2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetic acid as well as intermediates and processes for making the intermediates. Also provided are crystalline forms of the compound and the intermediates.
    Type: Grant
    Filed: May 24, 2016
    Date of Patent: January 2, 2018
    Assignee: Amgen Inc.
    Inventors: Matthew Bio, Sebastien Caille, Brian Cochran, Yuanqing Fang, Filisaty Vounatsos, Sarah Wortman
  • Substituted berbines and processes for their synthesis
    Patent number: 9856251
    Abstract: The present invention provides processes for the synthesis of substituted berbine compounds. Also provided are intermediates used in the synthesis of substituted berbine compounds.
    Type: Grant
    Filed: August 12, 2016
    Date of Patent: January 2, 2018
    Assignee: Mallinckrodt LLC
    Inventors: Peter X. Wang, Frank W. Moser, Gary L. Cantrell, Christopher W. Grote
  • Process for making 2-chloro-5-methylpyridine
    Patent number: 9850208
    Abstract: Processes for the preparation of 2-chloro-5-methylpyridine are described.
    Type: Grant
    Filed: January 27, 2015
    Date of Patent: December 26, 2017
    Assignee: Vertellus Holdings LLC
    Inventors: Ramiah Murugan, Martin Grendze
  • Process of preparing 3-(3-(4-aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-B]pyridin-2-YL)pyridin-2-amine
    Patent number: 9834556
    Abstract: The present invention is directed to a processes for the synthesis of 3-(3-(4-(1-aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine:
    Type: Grant
    Filed: September 7, 2016
    Date of Patent: December 5, 2017
    Assignee: ArQule, Inc.
    Inventors: Craig Bates, Jian-Xie Chen, Jianmin Mao, David P. Reed
  • Heterocyclic compounds and uses thereof
    Patent number: 9822109
    Abstract: Heterocyclic compounds of formula (I), methods for their preparation, pharmaceutical compositions containing such a compound and their therapeutic uses.
    Type: Grant
    Filed: September 4, 2015
    Date of Patent: November 21, 2017
    Assignee: Plexxikon Inc.
    Inventors: Jiazhong Zhang, Wayne Spevak
  • Bicyclic heteroaromatic carboxamide compounds useful as Pim kinase inhibitors
    Patent number: 9822124
    Abstract: The present disclosure describes bicyclic heteroaromatic carboxamide derivatives, as well as their compositions and methods of use. The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.
    Type: Grant
    Filed: July 13, 2015
    Date of Patent: November 21, 2017
    Assignee: Incyte Corporation
    Inventors: Oleg Vechorkin, Yun-Long Li
  • Bicyclic heteroaryl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
    Patent number: 9822118
    Abstract: Compounds of Formula I or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis and pelvic pain syndrome.
    Type: Grant
    Filed: November 13, 2013
    Date of Patent: November 21, 2017
    Assignee: Array BioPharma Inc.
    Inventors: Shelley Allen, Barbara J. Brandhuber, Kevin Ronald Condroski, Lily Huang, Timothy Kercher, Shannon L. Winski
  • Inhibitors of leukotriene A4 hydrolase
    Patent number: 9822106
    Abstract: The present invention is directed to compounds encompassed by the Formula (I), pharmaceutical compositions thereof, methods for inhibiting LTA-4 hydrolase, and methods for the treatment of a disease and disorder which is ameliorated by the inhibition of LTA4-h activity. Non-limiting examples of such diseases and conditions include inflammatory and autoimmune diseases and disorders.
    Type: Grant
    Filed: September 10, 2015
    Date of Patent: November 21, 2017
    Assignee: CELTAXSYS, INC.
    Inventors: William Guilford, David Davey
  • Inhibitors of the kynurenine pathway
    Patent number: 9815811
    Abstract: The present application provides novel inhibitors of indoleamine 2,3-dioxygenase-1 and/or indoleamine 2,3-dioxygenase-2 and/or tryptophan 2,3-dioxygenase, metabolites thereof, and pharmaceutically acceptable salts or prodrugs thereof. Also provided are methods for preparing these compounds. A therapeutically effective amount of one or more of the compounds of formula (I) is useful in treating diseases resulting from dysregulation of the kynurenine pathway. Compounds of formula (I) act by inhibiting the enzymatic activity or expression of indoleamine 2,3-dioxygenase-1 and/or indoleamine 2,3-dioxygenase-2 and/or tryptophan 2,3-dioxygenase.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: November 14, 2017
    Assignee: CURADEV PHARMA, PVT. LTD.
    Inventors: Monali Banerjee, Sandip Middya, Ritesh Shrivastava, Sushil Raina, Arjun Surya, Dharmendra B. Yadav, Veejendra K. Yadav, Kamal Kishore Kapoor, Aranapakam Venkatesan, Roger A. Smith, Scott K. Thompson